Substituted xanthines and methods of use thereof
Inventors
Chenard, Bertrand L. • Gallaschun, Randall J.
Assignees
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Publication Number
US-9969736-B2
Publication Date
2018-05-15
Expiration Date
Abstract
Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
Core Innovation
The invention relates to a method of therapeutically treating depression in a subject in need thereof by administering an effective amount of a compound or a pharmaceutically acceptable salt thereof. The administered compound is selected from specific purine-2,6(3H,7H)-dione derivatives with defined substituents at the 1-, 7-, and 8-positions.
The compounds share a purine-2,6(3H,7H)-dione scaffold and include 1-(3-hydroxypropyl) or 1-(4-hydroxybutyl) substituents, 7-(4-chlorobenzyl) or 7-((6-methylpyridin-3-yl)methyl) substituents, and 8-(3-(trifluoromethoxy)phenoxy) or 8-(3-chlorophenoxy) substituents. The disclosed set also includes related purine-based structures bearing substituted phenoxy, benzyl, and heteroaryl motifs.
The document further describes substituted purine-2,6-dione derivatives and their preparation and characterization, including related analogs with phenoxy and aryl ether substitution, hydroxyalkyl side chains, and fluorinated or chlorinated aromatic groups. The compounds are presented as candidate therapeutic agents for depression, and the partial content includes analytical characterization such as LCMS and 1H NMR for the described compounds and intermediates.
Claims Coverage
The independent claim covers a method of therapeutically treating depression by administering an effective amount of a selected purine-based compound or a pharmaceutically acceptable salt. The claim set includes four specifically enumerated compound structures, and a dependent claim further limits the depression subtype.
Therapeutic depression treatment with selected purine-2,6(3H,7H)-dione derivatives
A method of therapeutically treating depression in a subject in need thereof by administering an effective amount of a compound or a pharmaceutically acceptable salt, wherein the compound is selected from the group consisting of the specified substituted purine-2,6(3H,7H)-dione structures.
Hydroxyalkyl, chlorobenzyl, pyridinylmethyl, and phenoxy substitution on the purine core
The administered compounds include the listed combinations of 7-(4-chlorobenzyl), 1-(3-hydroxypropyl) or 1-(4-hydroxybutyl), 7-((6-methylpyridin-3-yl)methyl), and 8-(3-(trifluoromethoxy)phenoxy) or 8-(3-chlorophenoxy) substituents on the purine-2,6(3H,7H)-dione core.
Depression subtype selection
The depression is selected from the group consisting of major depression, psychiatric depression, dysthymia, and postpartum depression.
Overall, the claim coverage is centered on treating depression by administering an effective amount of one of four explicitly listed substituted purine-2,6(3H,7H)-dione compounds or pharmaceutically acceptable salts, with a dependent limitation to specified depression subtypes.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Therapeutically treating depression in a subject in need thereof by administering an effective amount of a selected substituted purine-2,6-dione compound or pharmaceutically acceptable salt.
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